Verapamil (0.17 microg kg(-1) min(-1) intravenous, i.v.) but not elgodipine (35 ng kg(-1) min(-1)) modestly enhanced the weak blood glucose increase induced by the i.v. infusion of isoprenaline (0.3 microg kg(-1) min(-1)) in conscious rabbits. However, elgodipine but not verapamil suppressed the increase in circulating insulin evoked by the agonist. Both drugs enhanced the rise in plasma lactate mediated by isoprenaline but only elgodipine potentiated the lipolytic effect of the agonist. In isolated islets elgodipine (10(-6) M) blocked forskolin (10(-6) M)-induced insulin release. However, in rabbit adipocytes elgodipine potentiated both glycerol release and cAMP accumulation induced by isoprenaline (10(-8)-10(-6) M). Excess K(+) (40-60 mM) did not alter basal lipolysis or the response to isoprenaline in either rabbit or mouse adipocytes. Therefore, Ca2+ influx through L-type Ca2+ channels does not seem to play a significant role in the lipolytic effect of isoprenaline. Metabolic alterations found with Ca2+ channel antagonists were of minor intensity and probably devoid of pathological implications.

01 Jan 1999·International journal of clinical pharmacology and therapeutics

Non-linear pharmacokinetic modelling of intravenous elgodipine.

Article

Author: Alberich, X ; Harrison, F ; de la Motte, S

OBJECTIVE, SUBJECTS AND METHODS: The 1,4-dihydropyridine elgodipine was given as continuous infusion at various rates (5, 10, 15, 20, 40 microg/kg/h for 48, 48, 48, 24, or 6 h, respectively) to five groups of 6-12 healthy male subjects (total 42). Elgodipine plasma concentrations were measured with HPLC in 20-24 samples from each subject. Concentrations increased overproportionally with dose. Non-compartmental and compartmental evaluations were made. A two-compartment model with lag time and Michaelis-Menten term for elimination was found to be appropriate.RESULTSBased on Michaelis-Menten parameters and concentration time courses during infusions, the elimination appeared to be saturated already at low dosages. There appeared to be two distinct subpopulations with two-fold differences in the maximal elimination velocity. In 9/42 subjects, more frequently in the groups with lower infusion rates, the model failed and the Michaelis-Menten term had to be replaced with a constant rate to fit. A dose-dependent increase in the volume of distribution and differences in and difficulties with estimations of the Michaelis-Menten constant KM might indicate a non-linear plasma protein binding. The transfer rate constants to or from the peripheral compartment correlated with blood hemoglobin or creatinine and bilirubin concentrations, respectively.CONCLUSIONThe results indicated that tissue distribution and protein binding had marked influence on the plasma concentrations and, thus, attenuated the impact of saturation in the elimination.

01 Sep 1998·European Journal of PharmacologyQ3 · MEDICINE

Characteristics of Ca2+ channel blockade by oxodipine and elgodipine in rat cardiomyocytes

Q3 · MEDICINE

Article

Author: Talavera, Karel ; Alvarez, Julio L. ; Vassort, Guy ; Galan, Loipa

The two novel dihydropyridines, oxodipine and elgodipine greatly depressed the KCl-induced contraction of rabbit aorta and decreased the cardiac force of contraction of rat ventricular strips with lower potency. Both compounds markedly shortened cardiac action potentials. In rat cultured neonatal ventricular myocytes, oxodipine and elgodipine decreased the L-type Ca2+ current (I(CaL)) with IC50 of 0.24 and 0.33 microM respectively while oxodipine was slightly more potent on the T-type Ca2+ current (I(CaT)) than elgodipine (IC50 = 0.41 vs. 2.18 microM). Both compounds were less potent in inhibiting I(CaL) of adult cardiomyocytes. Oxodipine exhibited mostly a tonic block of both currents while elgodipine induced mainly a use-dependent block. Oxodipine and elgodipine increased by at least one order of magnitude their inhibitory potency on I(CaT) and I(CaL) when the cells were partially depolarized. We conclude that the mechanisms of inhibition of Ca2+ channels by these two dihydropyridines are different and suggest that the underlying mechanism of vascular selectivity is the voltage-dependent block of I(CaL), with the use-dependent inhibition of Ca2+ currents by elgodipine further contributing to this selectivity.

100 Deals associated with Elgodipine

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Indication	Highest Phase	Country/Location	Organization	Date
Angina Pectoris	Phase 3	GB	-	-
Angina Pectoris	Phase 3	-	Iqb	-
Angina Pectoris	Phase 3	DE	-	-
Angina Pectoris	Phase 3	FR	-	-
Angina Pectoris	Phase 3	-	Almirall SA	-
Coronary Artery Disease	Phase 3	-	Almirall SA	-
Coronary Artery Disease	Phase 3	-	Iqb	-
Coronary Disease	Phase 3	GB	-	-
Angina Pectoris	Phase 2	ES	-	-
Coronary Disease	Phase 2	FR	-	-

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